129303-82-8Relevant academic research and scientific papers
Synthesis, SAR, and Pharmacological Characterization of Brain Penetrant P2X7 Receptor Antagonists
Savall, Brad M.,Wu, Duncan,De Angelis, Meri,Carruthers, Nicholas I.,Ao, Hong,Wang, Qi,Lord, Brian,Bhattacharya, Anindya,Letavic, Michael A.
, p. 671 - 676 (2015)
We describe the synthesis and SAR of 1,2,3-triazolopiperidines as a novel series of potent, brain penetrant P2X7 antagonists. Initial efforts yielded a series of potent human P2X7R antagonists with moderate to weak rodent potency, some CYP inhibition, poo
BICYCLIC HETEROCYCLIC DERIVATIVES
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, (2017/02/28)
Compounds of the formula la or of the formula lb in which X, Y, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases
P2X7 MODULATORS
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Paragraph 0440; 0441, (2014/09/29)
The present invention is directed to compounds of Formulas (I, IIa and IIb): The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, IIa and IIb). Methods of making and using the compounds of Formulas (I, IIa and IIb) are also within the scope of the invention.
